INTRODUCTION: Due to the role of bradykinin B1 receptor (B1R) in pain and inflammation, B1R antagonists have been suggested as promising drug candidates in chronic pain states. The first disclosed B1R antagonists were peptidomimetics, however, during the last few years, novel chemotypes with improved pharmacodynamic and pharmacokinetic properties have been identified.AREAS COVERED: In this review, we aim to give an overview on B1R antagonists published in patent applications between January 2009 and July 2012.EXPERT OPINION: Extensive research on B1R antagonists resulted in basically two chemotypes including sulfonamides and carboxamides. The most important achievement is that these scaffolds show improved PK profile relative to previous compounds. Several B1R antagonists entered clinical trials and the results from proof-of-concept Phase II clinical study is expected to be disclosed soon.